New generation broad-spectrum antibiotics: names

The first antimicrobial drug was discovered at the beginning of the 20th century. In 1929, London University professor Alexander Fleming began a detailed study of the properties of green mold and noted its special antibacterial properties. And in 1940, a pure culture of this substance was bred, which became the basis for the first antibiotic. This is how the well-known penicillin appeared, saving the lives of many people for almost 80 years.

Then the development of the science of antimicrobial agents proceeded on an increasing scale. More and more new effective antibiotics appeared, which had a destructive effect on microbes, inhibiting their growth and reproduction.

Working in this direction, microbiologists have discovered that some of the isolated antimicrobial substances behave in a special way. They exhibit antibacterial activity against several types of bacteria.

Preparations based on such substances of natural or synthetic origin, so beloved by doctors of various specializations, were called broad-spectrum antibiotics (BSAA) and have become no less widespread in clinical practice.

And yet, despite all the benefits of the above-mentioned drugs, they have one significant drawback. Their activity against many bacteria extends not only to pathogenic microorganisms, but also to those that are vital for the human body, forming its microflora. Thus, active use of oral antibiotics can destroy the beneficial intestinal microflora, causing disruption of its functioning, and the use of vaginal antibiotics can disrupt the acid balance of the vagina, provoking the development of fungal infections. In addition, the toxic effect of antibiotics of the first generations did not allow them to be used to treat patients with liver and kidney pathologies, to treat infectious diseases in childhood, during pregnancy and in some other situations, and a large number of side effects led to the fact that the treatment of one problem provoked the development of another.

In this regard, the question arose of finding solutions to the problem of how to make antibiotic treatment not only effective, but also safe. Developments began to be carried out in this direction, which contributed to the entry into the pharmaceutical market of a new product - effective broad-spectrum antibiotics of a new generation with fewer contraindications and side effects.

New generation antibiotic groups and development of antibiotic therapy

Among the large number of antimicrobial drugs (AMP), several groups of drugs can be distinguished that differ in chemical structure:

• Beta-lactams, which are divided into the following classes:
  • Penicillins
  • Cephalosporins
  • Carbapenems with increased resistance to beta-lactamases produced by some bacteria
• Macrolides (the least toxic drugs of natural origin)
• Tetracycline antibiotics
• Aminoglycosides, particularly active against gram-negative anaerobes that cause respiratory diseases
• Gastric-resistant lincosamides
• Antibiotics of the chloramphenicol series
• Glycopeptide drugs
• Polymyxins with a narrow spectrum of bacterial activity
• Sulfanilamides
• Quinolones, and in particular fluoroquinolones, have a broad spectrum of action.

In addition to the above groups, there are several more classes of narrowly targeted drugs, as well as antibiotics that cannot be assigned to a specific group. Also, several new groups of drugs have recently appeared, although they have a predominantly narrow spectrum of action.

Some groups and drugs have been familiar to us for a long time, others appeared later, and some are still unknown to the general consumer.

Antibiotics of the 1st and 2nd generations cannot be called ineffective. They are still used today. However, not only the person develops, but also the microbes inside him, acquiring resistance to frequently used drugs. In addition to acquiring a broad spectrum of action, the 3rd generation antibiotic was called upon to defeat such a phenomenon as antibiotic resistance, which has become especially relevant recently, and some 2nd generation antibiotics did not always cope with it successfully.

Antibiotics of the 4th generation, in addition to a wide spectrum of action, have other advantages. Thus, penicillins of the 4th generation are distinguished not only by high activity against gram-positive and gram-negative microflora, but, having a combined composition, they also become active against Pseudomonas aeruginosa, which is the causative agent of a large number of bacterial infections affecting various organs and systems of the human body.

Fourth generation macrolides are also combination drugs, where one of the active ingredients is a tetracycline antibiotic, which expands the field of activity of the drugs.

Particular attention should be paid to 4th generation cephalosporins, the spectrum of action of which is rightly called ultra-broad. These drugs are considered the strongest and most widely used in clinical practice, since they are effective against bacterial strains resistant to the effects of previous generations of AMP.

And yet, even these new cephalosporins are not without their drawbacks, as they can cause multiple side effects. The fight against this issue is still ongoing, so of all the known 4th generation cephalosporins (and there are about 10 varieties), only drugs based on cefpirome and cefepime are allowed into mass production.

The only 4th generation drug from the aminoglycoside group is capable of fighting such pathogenic microorganisms as Cytobacter, Aeromonas, Nocardia, which are not susceptible to drugs of earlier generations. It is also effective against Pseudomonas aeruginosa.

Broad-spectrum antibiotics of the 5th generation are mainly ureido- and piperazino-penicillins, as well as the only approved drug from the cephalosporin group.

Penicillins of the 5th generation are considered effective against gram-positive and gram-negative bacteria, including Pseudomonas aeruginosa. But their disadvantage is the lack of resistance to beta-lactamases.

The active component of the approved 5th generation cephalosporins is ceftobiprole, which has rapid absorption and good metabolism. It is used to combat strains of streptococci and staphylococci resistant to early generation beta-lactams, as well as various anaerobic pathogens. A feature of the antibiotic is that bacteria are not able to mutate under its action, which means that they do not develop antibiotic resistance.

Ceftaroline-based antibiotics are also highly effective, but they lack a protective mechanism against beta-lactamases produced by enterobacteria.

A new drug has also been developed based on a combination of ceftobiprole and tazobactam, which makes it more resistant to the effects of various types of beta-lactamases.

Antibiotics of the 6th generation of penicillin series are also not without a broad spectrum of action, but they show the greatest activity against gram-negative bacteria, including those that frequently prescribed 3rd generation penicillins based on amoxicillin cannot cope with.

These antibiotics are resistant to most beta-lactamase-producing bacteria, but are not without the side effects typical of penicillins.

Carbapenems and fluoroquinolones are relatively new types of antimicrobial drugs. Carbapenems are highly effective, resistant to most beta-lactamases, but they are not able to resist New Delhi metallo-beta-lactamase. Some carbapenems are not effective against fungi.

Fluoroquinolones are synthetic drugs with pronounced antimicrobial activity, which are similar in action to antibiotics. They are effective against most bacteria, including Mycobacterium tuberculosis, some types of pneumococci, Pseudomonas aeruginosa, etc. However, their effectiveness against anaerobic bacteria is extremely low.